Synthesisandanti-tobaccomosaicvirusactivityofoligopeptidechiralthioureascontainingphosphonatemoiety

In order to develop more effective anti-tobacco mosaic virus (TMV) agents, 18 noval oligopeptide chiral thioureas containing phosphonate moiety have been synthesized. Substituted benzylamines, amino acids and dialkyl phosphonate were employed as the starting materials. C-to-N synthesis strategy and coupling reagent O-benzotriazole-N,N,N′,N′-tetramethylurea(HBTU) were used. The structures of the target compounds were characterized by IR, (¹H, ¹³C, ³¹P, ¹⁹F) NMR and elemental analysis. The Anti-TMV activities of target compounds were evaluated for the first time. The results indicate that these compounds have a high therapeutic effect on TMV, and exhibit good anti-plant virus activities. The curative rates of 5i , 5j and 5p against TMV were 52.6%, 55.7% and 56.1%, respectively, which were comparable to the curative rate (55.4%) of the commercial reference ningnanmycin.